Jervine Hedgehog/Smoothened inhibitor

Cat.No.S4747

Jervine (11-Ketocyclopamine) is a Hedgehog signaling (IC50=500-700 nM) inhibitor that inhibits the sonic hedgehog (shh) pathway by interacting with smoothened.
Jervine Hedgehog/Smoothened inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 425.60

Quality Control

Cell Culture, Treatment & Working Concentration

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
s12 cells Function assay Inhibition of lipid-modified (octylated) form of SHH expressed in mouse s12 cells by luciferase reporter gene assay, IC50=0.5 μM
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight 425.60 Formula

C27H39NO3

Storage (From the date of receipt)
CAS No. 469-59-0 Download SDF Storage of Stock Solutions

Synonyms 11-Ketocyclopamine Smiles CC1CC2C(C(C3(O2)CCC4C5CC=C6CC(CCC6(C5C(=O)C4=C3C)C)O)C)NC1

Solubility

In vitro
Batch:

DMSO : 10 mg/mL (23.49 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 4 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
Hedgehog [1]
Shh [1]
In vitro
Compared to controls, chondrocyte cultures exposed to 25 μg/ml jervine shows an apparent reduction in cell number but no differences in cellular morphology or relative intensity of alcian blue staining[2].
In vivo
Embryos exposed to jervine develop craniofacial abnormalities related to those found in Shh mutant embryos. The lower jaw of these embryos is severely reduced in size, often leading to loss of the incisors. Treatment of pregnant mice with the hedgehog inhibitor jervine induces jaw defects in the embryos similar to those found in Prx1−/−Prx2−/− embryos. The distal part of the jaw is reduced in size, and both incisors are absent[1].
References

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Signaling Pathway Map